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含有piperazine和quinoxaline片段的flavonol衍生物:合成和抗真菌活性
Yi Liu1, Hui Xin1, Yuhong Wang1
1State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025, China.
Molecular diversity
|September 3, 2024
概括
新的黄醇衍生物显示出强大的抗真菌活性. 化合物N5可以有效地对抗Phomopsis sp. 和Phytophthora capsica,在植物保护试验中表现优于商业真菌杀菌剂阿佐克西斯特罗宾.
科学领域:
- 药用化学 医学化学
- 植物病理学 植物病理学
- 有机合成 有机合成
背景情况:
- 真菌病对农业构成重大威胁,需要开发新型抗真菌剂.
- 黄醇衍生物是具有潜在生物活性的一类有前途的化合物.
研究的目的:
- 设计和合成新型的黄醇衍生物,其中包括皮佩拉津和昆素部分.
- 为了评估这些合成化合物对关键植物病原菌的抗真菌功效.
主要方法:
- 目标黄衍生物的化学合成.
- 在体外对各种真菌进行抗真菌活性测试,包括Phomopsis sp. 和Phytophthora capsica. 这种类型的植物.
- 在果和叶的体内保护和治疗活性测定.
- 扫描电子显微镜 (SEM) 用于观察真菌菌的形态变化.
- 生物化学测定测量相对导电性和马隆迪化物 (MDA) 含量.
主要成果:
- 一些合成的化合物表现出显著的抗真菌活性.
- 化合物N5显示出对Phomopsis sp.的更高的疗效. (EC50 = 12.9 微克/毫升) 和Phytophthora capsica (EC50 = 25.8 微克/毫升),超过了阿佐克西斯特罗宾.
- 与阿佐克西斯特罗宾相比,N5对基维果和叶感染的保护性 (85.9%) 和治疗性 (67.0%) 活动有所增强.
- SEM和生物化学分析表明,N5破坏真菌细胞膜的完整性,并影响菌株生长.
结论:
- 合成的黄醇衍生物,特别是N5,代表了一种有前途的新型农业杀菌剂.
- N5的作用机制包括破坏致病性真菌细胞膜.
- 进一步调查N5作为潜在的农业化学品是有必要的.
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